Ektor
Bluelighter
Opiates/Opioids' affinity for each receptor, μ κ δ Lets build a table/chart!!!!
There are many opiate users, and there are many opiates and opioids too.
There are three main Opioid receptors, each with its different effect, a little summary could be:
- μ - Mu = Analgesia, Euphoria, Sedation, Miosis, Respiratory Depression, Costipation
- κ - Kappa =Perceptual Distortions, Dysphoria, Analgesia, Psychedelia/Delirium/Dissociation, Miosis
- δ - Delta =Antidepressant Effect, Analgesia, Convulsions
Every opioid will have some degree of affinity for some of these receptors and the effect it gives will depend onto which receptor it has affinity, how much affinity it has for each receptor, the fact if it is an Agonist, a Partial Agonist, an Antagonist or an Inverse Agonist and its Intrinsic Activity(Efficacy) in case it is a PA.
The most used opiate in the world is Heroin, which actually seems just to be a pro-drug to the long known Morphine, then there are the two most used opioids for the treatment of Heroin addiction, Methadone and Buprenorphine. It would be nice to know also the different affinities to each receptor of the two main used opioid antagonists, Naloxone and Naltrexone.
I would like to make a table with the different affinities and activities of the opioid i mentioned (you can suggest other ones if you have data), sadly i cant have access to full articles on academic websites for the moment, i only have access to abstracts, with usually don't contain much quantitative data.
HERE IS WHERE YOU CAN HELP! Suggest and write in your posts the different affinities and activities of these opioid to each receptor, i will edit my post to add your data in the chart that i will make here in the first post to be well visible to anyone who open this thread!
Edit: "When i put (-) or (+) after a substance called "Antagonist" it is to clarify if said chemical at that receptor behaves as a very low Efficacy partial agonist: (+), or as a very low Efficacy inverse agonist. If instead i put this symbol (0) it means the substance is believed to be a true Silent Antagonist or its antagonistic properties are not specified. As i'm starting to realize that terms like "Silent Antagonist" or "Full Agonist" are only great approximations, we can only put our best to make Science closer to Common Sense and Understanding of Life."
MORPHINE (HEROIN)
- μ - Mu = Affinity: 4.55nM Activity: Agonist, Efficacy: 75%
- κ - Kappa = Affinity: 26.9nM Activity: Agonist
- δ - Delta = Affinity: 217nM Activity: Agonist
METHADONE
- μ - Mu = Affinity: 3.16nM Activity: Agonist, Efficacy: 77%
- κ - Kappa = Affinity: ≈500/1'000nM aka Negligible Effect
- δ - Delta = Affinity: ≈500/1'000nM aka Negligible Effect
BUPRENORPHINE
- μ - Mu = Affinity: 0.9nM Activity: Partial Agonist, Efficacy: 34%
- κ - Kappa = Affinity: 0.71nM Activity: Antagonist (0)
- δ - Delta = Affinity: 3.7nM Activity: Antagonist (+)
NALOXONE
- μ - Mu = Affinity: 1.2nM Activity: Antagonist (-)
- κ - Kappa = Affinity: 12nM Activity: Antagonist (-)
- δ - Delta = Affinity: 19nM Activity: Antagonist (-)
NALTREXONE
- μ - Mu = Affinity: 0.39nM Activity: Antagonist (-)
- κ - Kappa = Affinity: 1.75nM Activity: Antagonist (-)
- δ - Delta = Affinity: 26.6nM Activity: Antagonist (-)
CODEINE
- μ - Mu = Affinity: 105nM Activity: Agonist
- κ - Kappa = Affinity: 15000nM Activity: Agonist
- δ - Delta = Affinity: 9300nM Activity: Agonist
OXYCODONE
- μ - Mu = Affinity: ≈23.4nM Activity: Agonist
- κ - Kappa = Affinity: ≈1560nM Activity: Agonist
- δ - Delta = Affinity: ≈982nM Activity: Agonist
There are many opiate users, and there are many opiates and opioids too.
There are three main Opioid receptors, each with its different effect, a little summary could be:
- μ - Mu = Analgesia, Euphoria, Sedation, Miosis, Respiratory Depression, Costipation
- κ - Kappa =Perceptual Distortions, Dysphoria, Analgesia, Psychedelia/Delirium/Dissociation, Miosis
- δ - Delta =Antidepressant Effect, Analgesia, Convulsions
Every opioid will have some degree of affinity for some of these receptors and the effect it gives will depend onto which receptor it has affinity, how much affinity it has for each receptor, the fact if it is an Agonist, a Partial Agonist, an Antagonist or an Inverse Agonist and its Intrinsic Activity(Efficacy) in case it is a PA.
The most used opiate in the world is Heroin, which actually seems just to be a pro-drug to the long known Morphine, then there are the two most used opioids for the treatment of Heroin addiction, Methadone and Buprenorphine. It would be nice to know also the different affinities to each receptor of the two main used opioid antagonists, Naloxone and Naltrexone.
I would like to make a table with the different affinities and activities of the opioid i mentioned (you can suggest other ones if you have data), sadly i cant have access to full articles on academic websites for the moment, i only have access to abstracts, with usually don't contain much quantitative data.
HERE IS WHERE YOU CAN HELP! Suggest and write in your posts the different affinities and activities of these opioid to each receptor, i will edit my post to add your data in the chart that i will make here in the first post to be well visible to anyone who open this thread!
Edit: "When i put (-) or (+) after a substance called "Antagonist" it is to clarify if said chemical at that receptor behaves as a very low Efficacy partial agonist: (+), or as a very low Efficacy inverse agonist. If instead i put this symbol (0) it means the substance is believed to be a true Silent Antagonist or its antagonistic properties are not specified. As i'm starting to realize that terms like "Silent Antagonist" or "Full Agonist" are only great approximations, we can only put our best to make Science closer to Common Sense and Understanding of Life."
MORPHINE (HEROIN)
- μ - Mu = Affinity: 4.55nM Activity: Agonist, Efficacy: 75%
- κ - Kappa = Affinity: 26.9nM Activity: Agonist
- δ - Delta = Affinity: 217nM Activity: Agonist
METHADONE
- μ - Mu = Affinity: 3.16nM Activity: Agonist, Efficacy: 77%
- κ - Kappa = Affinity: ≈500/1'000nM aka Negligible Effect
- δ - Delta = Affinity: ≈500/1'000nM aka Negligible Effect
BUPRENORPHINE
- μ - Mu = Affinity: 0.9nM Activity: Partial Agonist, Efficacy: 34%
- κ - Kappa = Affinity: 0.71nM Activity: Antagonist (0)
- δ - Delta = Affinity: 3.7nM Activity: Antagonist (+)
NALOXONE
- μ - Mu = Affinity: 1.2nM Activity: Antagonist (-)
- κ - Kappa = Affinity: 12nM Activity: Antagonist (-)
- δ - Delta = Affinity: 19nM Activity: Antagonist (-)
NALTREXONE
- μ - Mu = Affinity: 0.39nM Activity: Antagonist (-)
- κ - Kappa = Affinity: 1.75nM Activity: Antagonist (-)
- δ - Delta = Affinity: 26.6nM Activity: Antagonist (-)
CODEINE
- μ - Mu = Affinity: 105nM Activity: Agonist
- κ - Kappa = Affinity: 15000nM Activity: Agonist
- δ - Delta = Affinity: 9300nM Activity: Agonist
OXYCODONE
- μ - Mu = Affinity: ≈23.4nM Activity: Agonist
- κ - Kappa = Affinity: ≈1560nM Activity: Agonist
- δ - Delta = Affinity: ≈982nM Activity: Agonist
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